Estrogenic activity of estradiol and its metabolites in the ER-CALUX assay with human T47D breast cells

A number of metabolites of 17beta-estradiol were tested for their estrogenic activity using the ER-CA-LUX assay based on the increased expression of luciferase in exposed T47D breast cancer cells. E2beta and estrone showed similar potencies in the test, whereas E2alpha was 100 times less active. Inc...

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Published in:APMIS : acta pathologica, microbiologica et immunologica Scandinavica microbiologica et immunologica Scandinavica, 2001-02, Vol.109 (2), p.101-107
Main Authors: HOOGENBOOM, L. A. P., DE HAAN, L., HOOIJERINK, D., BOR, G., MURK, A. J., BROUWER, A.
Format: Article
Language:English
Subjects:
Biological and medical sciences
catecholestrogens
ER-CALUX
estradiol
Estradiol - metabolism
Estradiol - pharmacology
estradiol-esters
Estrogenicity
Estrogens, Catechol - metabolism
Estrone - metabolism
Gynecology. Andrology. Obstetrics
Humans
Mammary gland diseases
Medical sciences
Tumor Cells, Cultured
Tumors
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Summary:A number of metabolites of 17beta-estradiol were tested for their estrogenic activity using the ER-CA-LUX assay based on the increased expression of luciferase in exposed T47D breast cancer cells. E2beta and estrone showed similar potencies in the test, whereas E2alpha was 100 times less active. Incubation of cells with estrone (0.35 microM) resulted in the formation of E2beta, whereas the reverse reaction was observed for E2beta. The resulting equilibrium may explain the similar estrogenic potency of estrone in the test. The synthetic 17-hydroxy benzoate ester of E2beta was 3 times less active than the parent compound. The 17-hydroxy palmitate and oleate esters of E2beta, were respectively 25 and 200 times less active than the parent compound. The 2-hydroxy metabolites of E2beta and estrone showed a 5,000 to 10,000 fold lower activity. The 4-hydroxy metabolites were more potent than the 2-hydroxy metabolites, showing only a 20-200 times lower activity. The 2- and 4-methoxyesters of estrone were 700 times less active. It is concluded that the estrogenic potency of metabolites formed in cattle after treatment with E2beta, like estrone, E2alpha and especially the esters of E2beta, may be significant with respect to the potential risk of the use of estradiol for growth promotion in domestic animals in certain countries.
ISSN:0903-4641
1600-0463
DOI:10.1034/j.1600-0463.2001.d01-110.x